Development and Characterization of a Self-Emulsifying Drug Delivery System (Smedds) of Rilpivirine HCL

Patel, Rakshit; Soniwala, Moinuddin; Shah, Ketul

doi:10.7897/2230-8407.100131

Cited by 2 publications

(2 citation statements)

References 8 publications

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“…It increases the activity of extrahepatic lipoprotein lipase, resulting in the lipolysis process [21]. Gem activates peroxisome proliferator-activated receptor-alpha transcriptor factor ligand, a receptor that is involved in the metabolism of carbohydrates and fats and also in adipose tissue distribution [22]. This results in increased synthesis of lipoprotein lipase thereby increasing the clearance of triglyceride.…”

Section: Introductionmentioning

confidence: 99%

Formulation and Optimization of Nanosuspension for Improving Solubility and Dissolution of Gemfibrozil

Deshkar

Sonkamble

Mahore

2019

Asian J Pharm Clin Res

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Objective: The study aims at the formulation and optimization of gemfibrozil (Gem) nanosuspension (NS) for improving its solubility and dissolution rate.Method: Gem NS was prepared by precipitation-ultrasonication method using ethanol as solvent, water as anti-solvent, and polyvinyl alcohol (PVA) as a stabilizer. A Box–Behnken design was employed to study the effect of the independent variables, Gem concentration in the organic phase (X1), PVA concentration (X2) and sonication time (X3) on the dependent variable, drug release after 90 min (Y). The resulting data were statistically analyzed and subjected to 3D response surface methodology to study the influence of variables on the response. NS was evaluated for particle size, zeta potential, solubility and in vitro drug release and characterized using Fourier transform infrared spectroscopy (FTIR), differential scanning calorimetry (DSC), and X-ray diffractometry (XRD).Results: On the basis of the evaluation, NS4 formulation (with 80 mg/ml Gem, 0.5% PVA concentration, and 20 min of sonication time) demonstrated highest drug content with a particle size of 191.0 nm and zeta potential of −12.0 mV. Dissolution profiles of NS indicated 2.5-fold increase in drug release than pure drug. NS demonstrated 5- and 9-fold increase in solubility, in water, and phosphate buffer (pH 7.5), respectively, pure drug. DSC and XRD studies indicated changes in the crystallinity of Gem during NS formulation. No chemical change was evident in NS as indicated by FTIR.Conclusion: Gem NS formulation could serve as a promising approach for improving its solubility and dissolution rate.

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Section: Introductionmentioning

confidence: 99%

Formulation and Optimization of Nanosuspension for Improving Solubility and Dissolution of Gemfibrozil

Deshkar

Sonkamble

Mahore

2019

Asian J Pharm Clin Res

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“…It increases the activity of extrahepatic lipoprotein lipase, resulting in the lipolysis process 6 . Gem activates peroxisome proliferator-activated receptor-alpha transcriptor factor ligand, a receptor that is involved in the metabolism of carbohydrates and fats and also in adipose tissue distribution 7 . This results in increased synthesis of lipoprotein lipase thereby increasing the clearance of triglyceride.…”

Section: Introductionmentioning

confidence: 99%

Formulation, Development and Evaluation of Bilayer Floating Tablet of Gemfibrozil

Gufran¹,

Ghatuary²,

Shende³

et al. 2019

J. Drug Delivery Ther.

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Formulation development is an important part of drug design and development. Bioavailability and bioequivalence are totally dependent on formulation development. Now-a-days formulation development is done by following QbD (Quality by Design).The aim of present study is to formulate Gemfibrozil (Gem) sustained release (SR) and immediate release (IR) bilayer tablet by different concentration of Hydroxypropyl methylcellulose (HPMC) and HPMC K 100 M to control the release pattern. The sustained release layer of Gem was prepared by using different grades of HPMC like, HPMC K-15, HPMC K-4 along with other excipients by direct compression technique. The immediate release layer of Gem was prepared by Cross carmellose sodium, Crospovidone and Sodium starch glycolate by direct compression technique. The powders were evaluated for their flow properties and the finished tablets were evaluated for their physical parameters. The both immediate release and sustained release layers of Gem were characterized by FT-IR and in vitro dissolution studies. The drug release study of Gem was evaluated using USP-II paddle type dissolution apparatus. The release rate of Gem in immediate release layer was studied for 15 min in 0.1 N HCL media and that of Gem in sustained release layer was studied for 12 h in 0.1 N HCL. From the nine batches F6 batch showed good release behaviour 99.85% of drug is released over 12 hours. Gem belongs to BCS Class II (log P 3.6) with poor solubility and high permeability resulting in limited and variable bioavailability. Total four trial batches of each drug have been manufactured to optimize and develop a robust and stable formulation, the stability studies of the products also comply with ICH guideline. Keywords: Bilayer floating tablets, Gemfibrozil, Biphasic drug release, HPMC K 15.

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Development and Characterization of a Self-Emulsifying Drug Delivery System (Smedds) of Rilpivirine HCL

Cited by 2 publications

References 8 publications

Formulation and Optimization of Nanosuspension for Improving Solubility and Dissolution of Gemfibrozil

Formulation and Optimization of Nanosuspension for Improving Solubility and Dissolution of Gemfibrozil

Formulation, Development and Evaluation of Bilayer Floating Tablet of Gemfibrozil

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